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CGP 13501
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
CGP 13501图片
CAS NO:56189-68-5
包装与价格:
包装价格(元)
10mg电议
50mg电议

产品介绍
Positive modulator of GABAB receptors,allosteric
Cas No.56189-68-5
化学名3-(3,5-di-tert-butyl-4-hydroxyphenyl)-2,2-dimethylpropanal
Canonical SMILESCC(C)(C1=C(O)C(C(C)(C)C)=CC(CC(C)(C=O)C)=C1)C
分子式C19H30O2
分子量290.44
溶解度<29.04mg/ml in DMSO;<29.04mg/ml in ethanol
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

CGP 13501 is a positive allosteric modulator of GABAB receptor [1].

The GABAB receptor is a metabotropic transmembrane receptors for GABA that is linked via G-protein to potassium channel. It stimulates the opening of K+ channel and hyperpolarize the neuron.

CGP 13501 is a positive allosteric modulator of GABAB receptor. In Chinese hamster ovary (CHO) cell line expressing GABAB(1b/2), CGP 13501 potentiated GABA-stimulated GTPγ[35S] binding to cell membranes [1]. In rat cortex, CGP13501 (10 μM) enhanced GABA-mediated activation of Gαo and increased GTPγ[35S] binding in the presence of GABA. Also, in the hippocampus and cerebellum, CGP13501 increased GABA-induced GTPγ[35S] binding and activation of Gαo. In rat cortex, hippocampus and cerebellum, CGP55845A blocked the influence of CGP13501 on GABA-induced GTPγ[35S] binding at Gαo with pIC50 values of 7.4, 7.31 and 6.82, respectively. In cells expressing GABAB(1b+2) receptors, CGP13501 increased GTPγ[35S] binding at Gαi1/3 [2].

References:
[1].  Urwyler S, Mosbacher J, Lingenhoehl K, et al. Positive allosteric modulation of native and recombinant gamma-aminobutyric acid(B) receptors by 2,6-Di-tert-butyl-4-(3-hydroxy-2,2-dimethyl-propyl)-phenol (CGP7930) and its aldehyde analog CGP13501. Mol Pharmacol, 2001, 60(5): 963-971.
[2].  Rasheed N, Ahmad A, Al-Sheeha M, et al. Neuroprotective and anti-stress effect of A68930 in acute and chronic unpredictable stress model in rats. Neurosci Lett, 2011, 504(2): 151-155.